CNS-5161 is an NMDA receptor antagonist which was under development for the treatment of neuropathic pain and cancer pain but was never marketed. It is taken by intravenously or transdermally.
CNS-5161 was under development by CeNeS Pharmaceuticals. It reached phase 2 trials prior to the discontinuation of its development.
Adverse Effects In humans, the drug was found to produce mild dissociative-like effects such as visual disturbances and derealization at assessed doses of 250 to 2,000μg intravenously in clinical trials. In addition, it produced pronounced and dose-limiting hypertension.
Pharmacology The drug is a highly potent and selective noncompetitive antagonist of the NMDA receptor via PCP site, with an affinity (Ki) of 1.8nM. It produces analgesic, anticonvulsant, and neuroprotective effects in rodents. There was also some dose-dependent mortality related to respiratory failure in rodents.
Chemistry The chemical synthesis of CNS-5161 and isotopologues has been described.
See also NMDA receptor antagonist Aptiganel (CNS-1102)
References
External links Hallucinogens You Probably Haven't Heard of: CNS 5161 - Nervewing - Blogger